CA2539361A1 - Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and an estrogen agonist/antagonist - Google Patents
Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and an estrogen agonist/antagonist Download PDFInfo
- Publication number
- CA2539361A1 CA2539361A1 CA002539361A CA2539361A CA2539361A1 CA 2539361 A1 CA2539361 A1 CA 2539361A1 CA 002539361 A CA002539361 A CA 002539361A CA 2539361 A CA2539361 A CA 2539361A CA 2539361 A1 CA2539361 A1 CA 2539361A1
- Authority
- CA
- Canada
- Prior art keywords
- phenyl
- methylene
- vitamin
- antagonist
- pharmaceutically acceptable
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 17
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
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Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/59—Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K31/593—9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Neurology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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PCT/IB2004/002900 WO2005027924A1 (en) | 2003-09-19 | 2004-09-06 | Pharmaceutical compositions and methods comprising combinations of 2-alkylidene-19-nor-vitamin d derivatives and an estrogen agonist/antagonist |
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US7122533B2 (en) * | 1999-11-29 | 2006-10-17 | The United States Of America As Represented By The Department Of Health And Human Services | Cosalane compounds and methods for their use |
US7053075B2 (en) * | 2003-11-25 | 2006-05-30 | Deluca Hector F | Methods for reducing body fat using vitamin D compounds |
JP2007512376A (ja) | 2003-11-25 | 2007-05-17 | ウイスコンシン アラムニ リサーチ ファンデーション | 肥満症の予防及び治療用ビタミンd類似体 |
US7563783B2 (en) * | 2005-02-11 | 2009-07-21 | Wisconsin Alumni Research Foundation | 2-methylene-19-nor-(20S-24S)-1α,25-dihydroxyvitamin-D2 |
DK1848442T3 (da) * | 2005-02-11 | 2012-05-29 | Wisconsin Alumni Res Found | 2-methylene-19-nor-(20s-24epi)-1alfa,25-dihydroxyvitamine-d2 |
EP1865965A4 (en) * | 2005-03-29 | 2010-06-02 | Wisconsin Alumni Res Found | 2-METHYLENE-19-NOR- (23S) -25-DEHYDRO-1-HYDROXYVITAMINE-D3-26,23-LACTONE AND 2-METHYLENE-19-NOR- (23R) -25-DEHYDRO-1-HYDROXYVITAMINE-D3- 26.23-lACTONE |
US7528122B2 (en) * | 2006-02-02 | 2009-05-05 | Wisconsin Alumni Research Foundation | Vitamin D analog—NEL, methods and uses thereof |
US7803789B2 (en) * | 2006-02-02 | 2010-09-28 | Wisconsin Alumni Research Foundation | Vitamin D analog—RAK, methods and uses thereof |
JP2009527479A (ja) * | 2006-02-17 | 2009-07-30 | アバロン ファーマシューティカルズ,インコーポレイテッド | ヒドロキシピペリジン誘導体とその使用 |
EP2141994A4 (en) * | 2007-04-26 | 2011-05-18 | Avalon Pharmaceuticals | POLYCYCLIC COMPOUNDS AND USES THEREOF |
AU2011232562B2 (en) * | 2010-03-23 | 2014-10-02 | Wisconsin Alumni Research Foundation | Diastereomers of 2-methylene-19-nor-22-methyl-1alpha,25- dihydroxyvitamin D3 |
CA2794006C (en) | 2010-03-23 | 2017-11-28 | Wisconsin Alumni Research Foundation | (20s)-2-methylene-19-nor-22-dimethyl-1.alpha.,25-dihydroxyvitamin d3 and (20r)-2-methylene-19-nor-22-dimethyl-1.alpha.,25-hydroxyvitamin d3 |
US8664206B2 (en) | 2010-03-23 | 2014-03-04 | Wisconsin Alumni Research Foundation | Diastereomers of 2-methylene-19-nor-22-methyl-1α,25-dihydroxyvitamin D3 |
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BE637389A (enrdf_load_stackoverflow) * | 1962-09-13 | |||
US3822287A (en) * | 1969-04-17 | 1974-07-02 | Rexall Drug Chemical | Process for preparation of substituted 3,4-(diphenyl)chromans |
EP0002097B1 (en) * | 1977-08-22 | 1981-08-05 | Imperial Chemical Industries Plc | Triphenylalkene derivatives, process for their preparation and pharmaceutical compositions containing them |
DE3046719C2 (de) * | 1980-12-11 | 1983-02-17 | Klinge Pharma GmbH, 8000 München | 1,1,2-Triphenyl-but-1-en-Derivate, Verfahren zu ihrer Herstellung und Arzneimittel |
US4418068A (en) * | 1981-04-03 | 1983-11-29 | Eli Lilly And Company | Antiestrogenic and antiandrugenic benzothiophenes |
GB2126576B (en) * | 1982-06-25 | 1985-06-19 | Farmos Group Limited | Alkane and alkene derivatives |
DE3762617D1 (de) * | 1986-09-11 | 1990-06-13 | Nat Res Dev | Tamoxifenderivate. |
US5086191A (en) * | 1991-05-28 | 1992-02-04 | Wisconsin Alumni Research Foundation | Intermediates for the synthesis of 19-nor vitamin D compounds |
RU2107512C1 (ru) * | 1991-06-05 | 1998-03-27 | Дзе Проктер Энд Гэмбл Компани | Фармацевтическая композиция для остеоиндукции, способ генерации новой кости |
TW366342B (en) * | 1992-07-28 | 1999-08-11 | Lilly Co Eli | The use of 2-phenyl-3-aroylbenzothiophenes in inhibiting bone loss |
EP0619306B1 (en) * | 1993-04-05 | 1996-09-11 | Wisconsin Alumni Research Foundation | 19-Nor-vitamin D3 compounds with substituent at 2-position |
US5478847A (en) * | 1994-03-02 | 1995-12-26 | Eli Lilly And Company | Methods of use for inhibiting bone loss and lowering serum cholesterol |
US7501441B1 (en) * | 1994-09-20 | 2009-03-10 | Eli Lilly And Company | Naphthyl compounds, intermediates, processes, compositions, and methods |
US5552412A (en) * | 1995-01-09 | 1996-09-03 | Pfizer Inc | 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis |
US5510357A (en) * | 1995-02-28 | 1996-04-23 | Eli Lilly And Company | Benzothiophene compounds as anti-estrogenic agents |
US5780497A (en) * | 1996-04-19 | 1998-07-14 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
US5985910A (en) * | 1996-04-19 | 1999-11-16 | American Home Products Corporation | 3- [4- (2- Phenyl-Indole-1-ylmethyl) Phenyl]- Acrylamides as estrogenic agents |
US5998402A (en) * | 1996-04-19 | 1999-12-07 | American Home Products Corporation | 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents |
US5880137A (en) * | 1996-04-19 | 1999-03-09 | American Home Products Corporation | 2-phenyl-1- 4-(amino-1-yl-alk-1-ynyl)-benzyl!-1H-indol-5-ols as estrogenic agents |
US6392071B1 (en) * | 1997-03-17 | 2002-05-21 | Wisconsin Alumni: Research Foundation | 26,27-homologated-20-EPI-2-alkylidene-19-nor-vitamin D compounds |
US6306844B1 (en) * | 1997-03-17 | 2001-10-23 | Wisconsin Alumni Research Foundation | Use of 2α-methyl-19-nor-20(S)-1α, 25-dihydroxyvitamin D3 to increase bone strength |
US5843928A (en) * | 1997-03-17 | 1998-12-01 | Wisconsin Alumni Research Foundation | 2-alkylidene-19-nor-vitamin D compounds |
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EP1301189A2 (en) * | 2000-07-14 | 2003-04-16 | Wisconsin Alumni Research Foundation | USE OF 2-METHYLENE-19-NOR-20(S)-1$g(a),25-DIHYDROXYVITAMIN D 3? TO INCREASE BONE STRENGTH |
CA2445922A1 (en) * | 2001-05-10 | 2002-11-21 | Merck & Co., Inc. | Estrogen receptor modulators |
US20030195175A1 (en) * | 2002-03-25 | 2003-10-16 | Deluca Hector F. | Use of carbon-2-modified-vitamin D analogs to induce the formation of new bone |
US7259143B2 (en) * | 2002-09-05 | 2007-08-21 | Wisconsin Alumni Research Foundation | Method of extending the dose range of vitamin D compounds |
-
2004
- 2004-09-06 EP EP04769299A patent/EP1667692A1/en not_active Withdrawn
- 2004-09-06 KR KR1020067005416A patent/KR20060040746A/ko not_active Ceased
- 2004-09-06 JP JP2006526713A patent/JP2007505881A/ja active Pending
- 2004-09-06 RU RU2006107652/15A patent/RU2331425C2/ru not_active IP Right Cessation
- 2004-09-06 CN CNB2004800268325A patent/CN100496501C/zh not_active Expired - Fee Related
- 2004-09-06 BR BRPI0414448-1A patent/BRPI0414448A/pt not_active Application Discontinuation
- 2004-09-06 WO PCT/IB2004/002900 patent/WO2005027924A1/en active Application Filing
- 2004-09-06 AU AU2004273658A patent/AU2004273658A1/en not_active Abandoned
- 2004-09-06 MX MXPA06003122A patent/MXPA06003122A/es not_active Application Discontinuation
- 2004-09-06 CA CA002539361A patent/CA2539361A1/en not_active Abandoned
- 2004-09-16 US US10/943,568 patent/US20050070512A1/en not_active Abandoned
- 2004-09-17 TW TW093128107A patent/TW200522967A/zh unknown
-
2006
- 2006-02-08 IL IL173621A patent/IL173621A0/en unknown
- 2006-02-10 ZA ZA200601237A patent/ZA200601237B/en unknown
- 2006-03-03 CO CO06021161A patent/CO5670328A2/es not_active Application Discontinuation
- 2006-04-18 NO NO20061702A patent/NO20061702L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
CN100496501C (zh) | 2009-06-10 |
EP1667692A1 (en) | 2006-06-14 |
BRPI0414448A (pt) | 2006-11-14 |
CN1852720A (zh) | 2006-10-25 |
MXPA06003122A (es) | 2006-05-31 |
WO2005027924A1 (en) | 2005-03-31 |
KR20060040746A (ko) | 2006-05-10 |
AU2004273658A1 (en) | 2005-03-31 |
CO5670328A2 (es) | 2006-08-31 |
NO20061702L (no) | 2006-06-19 |
JP2007505881A (ja) | 2007-03-15 |
TW200522967A (en) | 2005-07-16 |
US20050070512A1 (en) | 2005-03-31 |
IL173621A0 (en) | 2006-07-05 |
ZA200601237B (en) | 2007-05-30 |
RU2331425C2 (ru) | 2008-08-20 |
RU2006107652A (ru) | 2007-10-27 |
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EEER | Examination request | ||
FZDE | Discontinued |